期刊
THERANOSTICS
卷 13, 期 2, 页码 472-482出版社
IVYSPRING INT PUBL
DOI: 10.7150/thno.79452
关键词
radiolabeling; radiosynthon; fluorine-18; fluorothiophosphate; positron emission tomography probe
18F-labeled fluorothiophosphate (FTP) synthons with high radiochemical yields can be rapidly generated in reaction solutions using wet [18F]F- without the need for substrate pre-modification or lengthy radiosynthesis procedures. This simplified one-pot 18F-labeling method allows for the visualization and translation of a variety of biomolecules, making it valuable for modern positron emission tomography techniques.
Rationale: Conventional 18F-labeling methods that demand substrate pre-modification or lengthy radiosynthesis procedures have impeded the visualization and translation of numerous biomolecules, as biomarkers or ligands, using modern positron emission tomography techniques in vivo. Moreover, 18F-labeled biomolecules in high molar activity (Am) that are indispensable for sensitive imaging could be only achieved under strict labeling conditions. Methods: Herein, 18F-labeled fluorothiophosphate (FTP) synthons in high Am have been generated rapidly in situ in reaction solutions with < 5% water via nucleophilic substitution by wet [18F]F-, which required minimal processing from cyclotron target water. Results: Various 18F-labeled FTP synthons have been prepared in 30 sec at room temperature with high radiochemical yields > 75% (isolated, non-decay-corrected). FTP synthons with unsaturated hydrocarbon or activated ester group can conjugate with typical small molecules, peptides, proteins, and metallic nanoparticles. 337-517 GBq mu mol-1 Am has been achieved for 18F-labeled c(RGDyK) peptide using an automatic module with 37-74 GBq initial activity. Conclusion: The combination of high 18F-fluorination efficiency of FTP synthons and following mild conjugation condition provides a universal simplified one-pot 18F-labeling method for broad unmodified biomolecular substrates.
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